Professional Documents
Culture Documents
- Liquid preparations that contain one or more soluble chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents -Homogenous mixture that is prepared by dissolving a solid, liquid or gas in another liquid and represents a group of preparations in which the molecules of the solute or dissolved substance are dispersed.
Solutions
Types of Solutions
1. Solid Solution the solvent is solid a. Solid in solid Example: Cu + gold= 12 karat yellow gold b. Liquid in solid Example: Hg dissolved in Ag = amalgam c. Gas in solid Example: air dissolved in soap = floating soap 2. Liquid Solution the solvent is liquid a. solid in liquid Ex: salt in water b. Liquid in liquid Ex: alcohol and water c. Gases in liquid Ex: carbonated beverages
3. Gaseous Solutions the solvent is gas a. Solid in gas Example: sulfur in air b. Liquid in gas Example: water vapor in air c. Gas in gas Example: oxygenated air
3. Temperature heating a liquid also causes solution to take place more rapidly by increasing the frequency which solvent molecules collide with the surface of the dissolving mixture
Exothermic reaction solute gives off heat during the process of solution; solubility is decreased with an increase in temperature. Example: more soluble in cold than hot water Methyl cellulose and calcium salts such as Ca(OH)2 2. Molecular Structure The general rule: like dissolves like
3. Effects of other substance Example: Iodine is very slightly soluble in water but when added to a concentrated solution of KI dissolves immediately. 4. pH Many of the organic substances which are used medicinally are either weak acids or weak bases. And their aqueous solubility depend upon the pH of the solvent.
Examples of Weak Bases Alkaloids atropine,codeine, morphine Antihistamines diphenhydramine, tripelennamine Local anesthetics cocaine, procaine, tetracaine
Water and alcohol Solubilities Of some Selected Weak Acids, Weak Bases, and Their Salts Number of mL of Solvent Required To Dissolve 1 g of Drug Drug Atropine Atropine Sulfate Codeine Codeine Sulfate Codeine Phosphate Water 455 0.5 120 30 2.5 Alcohol 2 5 2 1,280 325
Morphine
Morphine Sulfate Phenobarbital Phenobarbital sodium Procaine Procaine HCl Sulfadiazine Sodium Sulfadiazine 2
5,000
16 1,000 1 200 1 13,000
210
565 8 10 soluble 15 sparingly soluble Slightly soluble
Very Soluble Freely soluble Soluble Sparingly soluble Slightly soluble Very slightly soluble Practically soluble or Insoluble
Compound
Formula
1430 275 25 15
Pyrocatechol
Pyrogallol C6H3(OH) 3
C6H4(OH) 2
1.7
2.3
2000 200 50
Inorganic Molecules
1. Monovalent cation and anion of an ionic compound are generally water soluble Examples: NaCl, LiBr, KI, NH4NO3
2. Only one of the two ions is monovalent compounds are water soluble Examples: BaCl2, MgI2, Na2SO4, Na3 PO4
3. Both ions are multivalent - poor water soluble. Examples: CaSO4, BaSO4, BiPO4 Exceptions: ZnSO4 and FeSO4 4. Common salts of alkali metals are usually water soluble Exception: Li2CO3
6. Nitrates, Nitrites, acetates, chlorates and lactates are generally water soluble Exceptions: silver and mercurous acetate 7. Sulfates, sulfites and thiosulfates are generally water soluble Exceptions: Calcium and Barium salts 8. Chlorides, bromides and iodides are water soluble Exceptions: salts of silver and mercurous ions
9. Acid salts corresponding to an insoluble salt will be more water soluble than organic salts. 10. Hydroxides and oxides of compounds other than alkali metal cations and the ammonium ion are generally water insoluble.
11. Sulfides are water insoluble except for their alkali metal salts 12. Phosphates, carbonates, silicates, borates and hypochlorites are water insoluble except for their alkali metal salts and ammonium salts
Organic Molecules
1. Molecules having 1 polar functional group soluble to the the total lengths of 5Cs 2. Molecules having branched chains are more soluble than the corresponding straight-chain compound. 3. Water solubility decreases with increase in MW 4. Increased structural similarity between solute and solvents accompanied by increase solubility.
4. Diluted Alcohol NF- prepared by mixing equal volume of Alcohol USP and purified water. 5. Alcohol, Rubbing contains about 70% of ethyl alcohol by volume the remainder consists of water, denaturants with or without color additives and perfume oils and stabilizers. 6. Glycerin USP ( Glycerol) clear syrupy liquid with sweet taste. It is miscible both with water and alcohol. Excellent solvent for tannins, phenol and boric acid. It has a preservative qualities. 7. Propylene Glycol miscible in water, acetone, alcohol and chloroform 8. Polyethylene glycol 400 miscible in water, acetone alcohol and other glycols 9. Chloroform miscible with alcohol, ether, benzene, hexane and both fixed and volatile oils 10. Acetone miscible with water, alcohol, ether, chloroform and most of the volatile oils.
Magnesium Citrate = prepared by reacting official magnesium carbonate with citric acid, flavoring and sweetening agents, filtering talc and carbonating it by potassium or sodium bicarbonate. Use: Saline cathartic Sodium Citrate and Citric acid oral solution = contains 100 mg sodium citrate and 67 mg citric acid in each ml od aqueous solution. Use: Systemic alkalinizer
3. Solution by Extraction vegetables or animal origin are often extracted with suitable solvent. Preparation of this type may be classified as solutions but more often EXTRACTIVES
Examples of Oral Solution by Category 1. Antidepressants Notriptylline HCl Pamelor Oral Solution Fluoxetine HCl Prozac Liquid 2. Antiperistaltic Diphennoxylate HCl and Atropine Sulfate- Lomotil Liquid Loperamide HCl- Immodium A-D Liquid 3. Bronchidilator Theophylline Theophylline Oral Solution 4. Antipsychotics Haloperidol Haldol Concentrate Perphenazine Trilafon Concentrate Thiothixene HCl Navane Concentrate
10. Hematinic
Ferrous Sulfate - Fer-in-sol Drops 11. Histamine hydrogen Antagonist Cimetidine HCl liquid Tagamet HCl Liquid 12. Narcotic Agonist Analgesic Methadone HCl Methadone HCl 13. Vitamin D source Ergocalciferol Calciferol drops
AQUEOUS SOLUTIONS
Is one where water is used as a major ingredient. Water is used as a vehicle and a solvent for the desired flavoring or medical agent.
CHARACTERISTICS OF WATER 1. Tasteless 2. Freedom from irritating qualities 3. Lack of pharmacologic activity DISADVANTAGES 1. Favorable medium for many chemical reactions 2. Support growth of microorganisms when contaminated 3. In pure form add cost to production
PREPARATION 1. Distillation 2. Demineralization or Deionization 3. Reverse Osmosis **Demineralization This ionization process is the well known Zeolite process of softening water high mineral content. This resin may be acid or cations exchanger and base or anion exchanger. Zeolite act as a catalyst such as dehydrated aluminum. Calcium sodium sulfate. * Deionization process do not necessarily produce purified water which will comply with USPHS ( US Public Health Service) requirements for drinking water, the water should be purified before they can used for pharmaceuticals
**Reverse Osmosis Transport of solvent through semipermeable membrane separating 2 solutions of different concentrations (less concentrated and more concentrated) A reversely new separation process w/c in principle may be applied to the separation, concentration and fractionalization of inorganic or organic substances in aqueous or non-aqueous solutions in the liquid or the gaseous phase is known reverse osmosis. Also referred as crossflow or tangential flow membrane filtration
PORE SIZE
1. Microfiltration (0.1 to 2 microns) = bacteria 2. Ultrafiltration (0.01 to 0.1 microns) = virus 3. Nanofiltration (0.001 to 0.01 microns) = organic compounds in the MW of 300 to 1000 4. Reverse Osmosis (smaller than 0.001 microns
AROMATIC WATERS
Aromatic water is also called medicated water, defined in the USP as clear, saturated aqueous solutions of volatile oils or other aromatic or volatile substances. These are to be free from 1. Smoke like odor and other odors 2. Must have odor and taste similar to those oil or drugs from which they are prepared. 2 Components 1. Volatile oil 2. Water
Formula: Peppermint oil 20mL 90%Ethanol 600mL Purified Talc 50g Purified Water q.s.to make 1000mL Uses: Vehicle for internal aqueous sol. Carminative, flavoring diluent Description: Clear, saturated solution
B. Alternate Solution by Intervention - The volatile material is mixed thoroughly with 15g of purified talc. -The mixture is agitated with purified water for ten minutes prior to filtration. - The disadvantage of this method is the fineness of the filter aid which passes through the filter paper.
AROMATIC WATER
Stability Aromatic water are not permanently stable preparations Preservation of Aromatic Water Protect from excessive light and heat. Deterioration may due to volatilization. Decomposition or mold growth producing cloudy preparation or disagreeable odor.
Cinnamon Water Preparation: Cinnamon Water Synonym: Casio Nare, Cassia Oil Latin Name: Aqua Cinnamoni Formula: Cinnamon oil 20mL Ethanol 90% 600mL Purified Talc 50g Purified water q.s. to make 1000mL Procedure: Alternate Solution Method Uses: As flavored vehicle for internal aqueous solution, antiseptic in eye lotion, carminative Description: Clear, Saturated Solution
AQUEOUS ACIDS
Inorganic and organic acids such as HCl, HNO3, HI, HBr, H2SO4, and Hac., of great importance in chemical and pharmaceutical manufacturing Division of inorganic acids 1. Hydroacids no oxygen 2. Oxygen containing acids
Uses: Bactericidal and occasionally used in 1% solution for surgical dressings of the skin; 1% spermatocidal, as vaginal douche Description: Clear, colorless, having a strong characteristic odor and sharply acid taste, miscible with water.
Examples of Official Acids Although Not All of them are Aqueous acids
1. Acetic Acid 2. Diluted Acetic Acid 3. Glacial Acetic Acid 4. Diluted Hydroiodic Acid 5. Diluted Hydrochloric Acid 6. Hypophosphorous Acid 7. Folic Acid 8. Citric Acid 9. Folic Acid 10. Phosphoric Acid 11. Tartaric Acid 12. Salicylic Acid
GARGLES
Are aqueous solutions used for treating the pharynx and nasopharynx by forcing air from the lungs through gargle which is held in the throat. Many gargles must be diluted with water prior to use.
Gargles
Examples: Phenol Gargle and Potassium Chlorate (also known as Golden Gargle) and Phenol Gargle are official in B.P.C Preparation: Phenol Gargle Synonym: Phenolic Solution, Carbolic gargle Latin name: Gargarisma Phenol Formula: Contains 50mL of Phenol Glycerin (16% w/w phenol and 84% w/w glycerin), 10mL amaranth solution(1%w/v in chloroform water) and water to make 1L. This is diluted with warm water equal volume before use . For external use Uses: antiseptic and soothing effect
Examples: 1. Dobells solution or compound Sodium Borate NF contains Sodium borate. Liquified Phenol and Glycerin and sodium Bicarbonate use: antiseptic 2. Compound Sodium Chloride Mouthwash Zinc sulfate and ZnCl2
Special Washes 1. Eye washes (Collyrium) - as anesthetic, antiinfective, diagnostic, myotic and antiinflammatory 2. Mouthwash (Collutorium)- antibacterial 3. Nasal wash ( Collunarium) - antibacterial and antiseptic
JUICES
Juices are formerly known as INPISSATED JUICES. A juice prepared from ripe fruit, aqueous in character, and it is used in making syrups employed as vehicle. Examples: Cherry juice and Raspberry juices are official in USP
SPRAYS
Aqueous solutions in the form of coarse droplets or as finely divided solids to be applied topically, most usually to the nasal- pharyngeal tract or to skin Applied to the mucous membrane of the nose and throat by means of an atomizer or nebulizer Such sprays may contain antibiotics, antihistamine, vasoconstrictor, alcohol and suitable solubilizing and wetting agents Another device to deliver spray is called spray-omizer, this is for throat Examples: Nasalide(Syntex), Nostrilla
COLLODIONS
Are liquid preparation composed by pyroxillin dissolved a solvent mixture. Usually composed of alcohol and ether with or without added substances Pyroxillin (nitrocellulose soluble gun cotton, collodion cotton) is obtained by the action of mixture of nitric acid and sulfuric acids on cotton and consists chiefly of cellulose tetranitrate.
2. As medication where a thin layer of the medication is firmly placed against the skin Direction Of Use
Collodion are applied to the skin by means of a soft brush or other suitable applicators. The solvent rapidly evaporates, leaving a film residue of pyroxillin.
A. Salicylic acid Collodion, USP is 10% solution of salicylic acid in flexible collodion. Used as keratolytic effect ( topical drug that softens the superficial keratin-containing layer of the skin and promotes its desquamation) especially in the removal of corns from the toes
Synonym: Corn solvent
Formerly called Essences alcoholic or hydroalcoholic solutions of volatile substances. First Spirits 1. Brandy Spiritus Vini vitis 48 to 54% alcohol from grapes 2. Whisky - Spiritus frumenti 47 to 53% of alcohol from cereals Uses: 1. As flavoring agents pharmaceutically 2. For therapeutic value of the aromatic solute medicinally
SPIRITS
Preparation of Spirits
1. Simple Solution
Majority of spirits are prepared by dissolving the solute in alcohol by agitation. Filtration is generally desirable to obtain a sparking clear product. Example: Aromatic Spirit - 62 to 68% hydroalcoholic solution of ammonia and ammonium carbonate flavored and perfumed with lemon, lavender and myristica oil.
Example: Peppermint Spirit (Spiritus Menthae Piperitae) 79 to 85% hydroalcoholic solution containing 10% peppermint oil Use: digestive aid or carminative
Preparation of Spirits
3. Solution by Chemical Reaction
Only the preparation of Aromatic Spirit of Ammonia NF, involves a chemical reaction where the official Ammonium carbonate
4. Distillation No spirits currently official are prepared by distillation, However, two products of historical significance which is official in NF are prepared by distillation. Examples: Brandy and whisky
TOOTHACHE DROPS
Are preparations used for the temporary relief of toothache by application of a small cotton saturated with the product into the tooth cavity Example: Clove oil and mixture of phenol with camphor or creosote
3. Carbamide Peroxide Dental anti-ineffective . Acts as chemomechanical cleansing and debriding agent through the release of bubbling oxygen. Commercial product GlyOxide - contains 10% carbamide in flavored anhydrous glycerin. 4. Cetylpyridinium Chloride Solution and Lozenges- Local anti-infective. Commercial counter parts. Cepacol Mouthwash/Gargles and Lozenges 5. Erythrosine Sodium Solution/tablets-Diagnostic Aid. Solution applied to the teeth to reveal plaque left by inadequate brushing. Tablets same purpose and are not to be swallowed. 6. Eugenol - Dental Analgesic. Applied to dental cavities and dental protectives
7. Lidocaine Oral Spray Topical dental anesthetic. Applied through metered spray in the amount of 10mg per spray. 8. Nystatin Oral Suspension Antifungal 9. Na Fluoride /Tablets - Dental carries prophylactic
10. Saliva Substitutes contains electrolytes in CMC base and indicated for the relief of drymouth and throat in xerostomia 11. Triamcinolone Acetonide Dental Paste Topical Anti-inflammatory 12. Zinc Oxide-Eugenol Mixtures A temporary filling mix
INHALATIONS
- drugs or solutions of drugs administered by the nasal or oral respiratory route.
- A widely used instrument capable of producing fine particles for inhalation therapy is the nebulizers =When volatile medication is added to the water in the chamber, the medication is volatilizes and also inhaled by the patient and Humidifiers will be used =The common household vaporizer produces a fine mist of steam that may be used to humidify a room will be used also Examples: 1. Isoetharine inhalation- bronchial asthma 2. Isoproterenol inhalation- bronchial asthma
INHALANTS
A drugs or combinations of drugs the by virtue of their high vapor pressure can be carried by a current into the nasal passage where they exert their effects.
SYRUPS
Syrups are concentrated solutions of sugar (such as sucrose) in water or other aqueous liquids with or without added flavoring agents and medicinal substances 3 Types of syrups 1. Simple syrup concentrated solution of sucrose in purified water alone. 2. Medicated syrup aqueous solution of sucrose containing other substances as polyols(glycerin and sorbitol) 3. Non-medicated/Flavored syrup contained various aromatic and pleasantly flavored substances and is intended as a vehicle or flavor for preparations.
Classification of syrups
A. Medicinal Classification 1. Non-medicated/Flavoring syrups are used as vehicles and have no official formulas and therefore no detailed descriptions of the product are found in compedia. B. Pharmaceutical Classification Based on their basic formula 1. sugar based syrups syrups which are concentrated solutions 2. artificial sweeteners and non-nutritive syrups formulated with artificial sweetening agents and viscosity builders
1. Orange Syrup - This sucrose - based syrup utilizes sweet orange peel tincture, and citric acid as the source of flavor and tartness.
Syrupus Aurantii, syrup of orange peel, sweet orange peel 50 mL;citric acid 5 g; talc 15 g; sucrose 820 g; purified water q.s to make 1000 mL 2. Ora - Sweet and Ora-Sweet SF -Commercially available vehicles for the extemporaneous compounding of Syrups. Ora sweet SF syrup is sugar free. 3.Raspberry Syrup - A sucrose - based syrup containing about 48% by volume of raspberry juice
4. Glycyrrhiza Syrup - Licorice syrup, Glycyrrhiza fluid extract 250 mL; Fennel oil 0.55 mL; Anise oil 0.5 mL; syrups, q.s to make 1000 mL
5. Cocoa Syrup - Syrupus cacao, Cacao syrup, chocolate flavored, cocoa 180 g; sucrose 600 g; liquid glucose 180 g; glycerin 50 mL; Sodium chloride 2 g; Vanilla 0.2 g; Sodium benzoate 1 g; water q.s. to make 1000 mL 6.Cherry Syrup - Syrupus Gerasi - Cherry juice 475 mL; sucrose 800 g; alcohol 20 mL; water q.s. to make 1000 mL 7. Acacia Syrup - Syrupus acaciae - Acacia powder 100g; Sodium benzoate 1 g; Vanilla tincture 5 mL; Sucrose 800 g; Purified water q.s to make 1000 mL. 8. Citric acid Syrup - Syrupus Acidi Citrici, Syrup lemon Lemon tincture 10 mL; Citric acid 10 g: Purified water q.s to make 1000 mL
9. Simple Syrup - This is an 85% of sucrose in purified water. This simple syrup may be used as the basis for the preparation of flavored or medicated syrup.
them
Example: Ephedrine Sulfate Syrup -(for cough) - Ephedrine sulfate 4 g; Citric acid 1 g;Amaranth solution 4 mL; Caramel 0.4 g; Lemon oil 0.125 mL; orange oil 0.25 mL; Benzaldehyde 0.06 mL; Vanillin 0.016 g; alcohol 25 mL; Sucrose 800 g; Purified water, q.s to make 1000 mL
Ipecac Syrup - emetic Note: Some syrup are use as Cathartic, Cholinergic, Decongestant, Expectorant, Fecal Softener, Sedative and others Examples Of Medicated Syrups By Category
3. Antiemetics Chlorpromazine HCl Syrup - Thorazine Syrup Dimenhydrinate Syrup - Childrens Dramamine Liquid Prochlorperazine Edisylate - Compazine Syrup
5. Antipsychotic
Lithium Citrate - Lithium Citrate Syrup 6. Antihistamines Chlorpheniramine Maleate - Chlor-Trimeton Cyproheptadine HCl - Periactin Syrup Hydroxyzine HCl - Atarax Syrup
12. Decongestant
0.4 g
25.0 mL 83.0 mL
Sorbitol Solution
Sodium Benzoate Alcohol Color and Flavor Purified water, to make
282.0 mL
1.0 g 60.0 mL q.s 1000.0 mL
Sodium Benzoate
Flavor Purified water, to make q.s
1.0 g
1000.0 mL
Sodium Chloride
Alcohol Sorbitol Solution Syrup Liquid Glucose Glycerin Color/Flavor Purified Water to make
5.2 g
50.0 mL 324.0 mL 132.0 mL 44.0 mL 50.0 mL q.s 1000.0 mL
Benzoic Acid
Disodium Calcium EDTA Propylene glycol
1.0 g
1.0 g 150.0 mL
Alcohol
Saccharin Sodium Purified water
150.0 mL
1.8 g 200.0 mL
Flavor
Sorbitol Solution, to make
q.s
1000.0mL
Components Of Syrups
1. Sugar - usually sucrose and other substitutes for sweetness and viscosity 2. Antimicrobial preservatives 3. Flavorants 4. Colorants 5. Miscellaneous - special solvents, solubilizing agents, thickeners or stabilizers
Preservation and Storage of Syrups Generally, syrups are stored at room temperature in tightly closed bottle and well-filled bottles. Antimicrobial Preservatives The amount of preservatives required in a syrup varies with the proportions of water available for microbial growth. Among the preservatives 1. Benzoic acid-0.1% to 0.2% 2. Sodium benzoate 0.1 to 0.2% 3. Combination of methyl, propyl, butyl parabens totaling 0.1%
DEXTROSE
Dextrose may be used as a substitute for sucrose in syrups containing strong acids in order to eliminate the discoloration associated with caramelization. Example: Hydroiodic syrup The difficulty or problem with dextrose are as follows: It forms a saturated solutions in water at 70%w/v which is less viscous than simple syrup. Dextrose dissolves more slowly Dextrose is less sweet Saturated solution supports growth of microorganism and therefore more easily fermented.
1. 2. 3. 4.
DEXTROSE
So with the use of dextrose, it is necessary to improve the keeping qualities by adding: 1. Preservatives which may be glycerin in 30 to 45% which is also serves to increase viscosity. 2. Sweeteners 3. However, glycerin tends to develop a butyric odor or aging Flavorants for syrup Most syrups flavored with synthetic flavorants or with naturally occurring materials as volatile oil, vanillin, and others, to render the syrup pleasant tasting. Since syrups are aqueous preparations, these flavorants must be possess sufficient water solubility
Sweeteners
Non-nutritive, synthetic sweetening agents required in the formulation Saccharin sodium is 300 - 550 time as sweet as sucrose. It may be used in concentration of 0.1 to 0.2% but characterized by a bitter after taste. Aspartylphenylalanine methyl ester is a potential low calories 160 times sweeter than sucrose in aqueous solution.
Sorbitol, A hexahydric alcohol, C6H14O6, made by hydrogenation of glucose is used mostly in the 70% aqueous solution USP trademark Sorbo Characteristics of Sorbitol
1. Sorbitol solution is not irritating to the membrane of the mouth and the throat 2. Unlike sucrose, it does not contribute to the formation of dental caries
3. Although it is metabolized and converted into glucose it is not absorbed from the GIT as rapid as sugars, so no significant hyperglycemia is formed
4. Although it is 60% as sweet as sucrose and half as viscous as simple syrup, it has excellent mouth feel and lacks acrid characteristics. 5. Sorbitol is compatible with other polyol and simple syrup 6. Sorbitol is chemically stable and practically inert. 7. Sorbitol inhibits the sticking and locking of bottle caps which occurs with high concentration of sucrose so they are usually combined 8. Many drugs are more stable in sorbitol than in sucrose solution thus may have extended shelf-life 9. As much as 10% v/v of alcohol can be added before crystallization is observed same as sucrose.
Uses Of Syrups 1. Due to sweetness, can mask the taste of salty and bitter drugs and therefore serve as pleasant tasting vehicle
2. Used as vehicle for pediatric use due to to their high viscosity and the smoothness and mouth feel qualities. 3. Due to the wide variety of flavors of syrups such as orange, lemon, peppermint, these are widely acceptable.
Preparation Of Syrups
Syrups are most frequently prepared by any one of the four methods depending upon the physical and chemical characteristics of the ingredients.
1. Solution of the ingredients with the aid of heat 2. Solution of the ingredients by agitation without the use of heat or the simple admixture of liquid components 3. Addition of sucrose to a prepared medicated liquid or to a flavored liquid 4. By percolation of either the sucrose of the medicating substance or of the sucrose.
1. Add the sugar to the purified water and heat until solution is affected.
2. Heat stable components are added to the hot syrup 3. Cool and made up to volume. 4. If other components are heat labile, they are added after cooling like alcohol and oil. Caution: Do not apply excessive heat - inversion of sucrose causing discoloration due to caramelization
Examples : Acacia syrup, NF; Cocoa Syrup, NF; Syrup USP (85% sugar, made by cold and hot process, percolation)
heat
To avoid heat-induced inversion of sucrose, a syrup maybe prepared without heat by agitation Procedure: 1. Sucrose and other formulative agents maybe dissolved in purified water. 2. Place the ingredients in a bottle of greater capacity than the volume of syrup. 3. Agitate the mixture Examples: Ferrous Sulfate Syrup, Ephedrine Sulfate, Citric acid Syrup, and Glycyrrhiza Syrup
3. Percolation
In this method, either sucrose maybe percolated to prepare the syrup or the sucrose of the medicinal component may be percolated to form an extractive to which sucrose or syrup may be added
Procedure:
1. Purified water or aqueous solution of a medicating or flavoring liquid is allowed to pass slowly through a column of crystalline sucrose to dissolve it.
2. The percolate is collected and returned to the percolator as required until all of the sucrose has been dissolved. 3. Percolator with a pledget of cotton at the bottom is used Example: Tolu Balsam syrup - flavor for cough syrup 4. Addition of Sucrose to a Medicated liquid or to a Flavored liquid is syrup. Occasionally, a medicated liquid, as a tincture of fluidextract employed as the source of medication in the preparation of a
Many such tinctures and fluidextract contain alcohol-soluble constituents and are prepared with alcoholic vehicles.
HONEY
Honey is also called Clarified honey or Strained Honey Honey instead of syrup was used as a base for thick liquid preparation known as Honeys or Mels. Honey is the secretion deposited in the honeycomb of the bee and consists of a mixture of invert sugar 6283%; sucrose 8%; dextrin 0.2% Examples: Oxymel (acid honey) contains acetic acid 150 mL; Purified water 150 mL; honey q.s to make 1000 mL Squill Oxymel = squill, water, acetic acid and honey
MUCILAGES
Are thick, viscid, adhesive liquids, produced by dispersing gum in water or by extracting with water mucilagenous principle from vegetable substances. Mucilages are used primarily to aid in suspending insoluble substances in liquids due to their 1. colloidal character 2. viscosity which prevents the immediate sedimentation
Example:
Preparation: Acacia Mucilage NF Synonym: Mucilago Acaciae; Mucilage of Gum Arabic Formula : Acacia, in small fragments Benzoic acid Purified water, q.s to make 350 g 2g 1000 mL
Method: Place acacia in wide mouth graduated bottle with capacity not exceeding 1000 mL. Wash the drug with cold water, drain and add sufficient quantity of purified water in which benzoic acid has been dissolved to make 1000 mL, Stopper and lay the bottle, rotate occasionally, and when acacia has been dissolved, strain the mucilage Uses: Demulcent, suspending agent, excipient in making pills and troches,and as emulsifying agent for cod liver oil
Example:
Preparation: Tragacanth Mucilage NF Synonym: Mucilago Tragacanthae Formula : Tragacanth 6.0 g
Benzoic acid
Glycerin
0.2 g
18.0 g
Method : Mix 75 mL of purified water with glycerin in a tared vessel, heat to boiling, discontinue application of heat, add Tragacanth and the Benzoic acid and macerate during 24 hours, stirring occasionally. Add sufficient quantity of purified water to make the mucilage 100 g, stir actively until uniform consistency and strain through muslin cloth
Uses: excipient for pills or troches, suspending agent for insoluble substances for internal mixtures and as protective agent
ELIXIRS
Are clear, pleasantly flavored, sweetened hdyroalcoholic liquids intended for oral as compared to syrup, elixirs are less sweet and viscous since they contain a lower portion of sugar and consequently less effective in masking the taste of medicinal substances
Advantages of elixirs
1. Because of their hydroalcoholic character, elixirs are better able than the aqueous syrups to maintain both water soluble and alcohol soluble components in the solutions 2. More preferred than syrups due to the stability character
3. Easy to prepare which is by simple solution 4. Pleasant flavor
Characteristics of Elixir
1. The main ingredient of elixirs are ethanol and water but glycerin sorbitol, propylene glycol, flavoring agents, preservatives and syrups are often used in preparation of the final product 2. The alcohol content vary from 3 to 41% depending on the water alcohol solubility of the ingredients 3. Although many elixirs are sweetened with sucrose, some utilize sorbitol, glycerin, and artificial sweeteners such as saccharin for this purpose. 4. Elixirs having a high alcoholic content usually use as artificial sweeteners as saccharin which is used in small quantities only.
Preparation of Elixirs 1. Simple solution with agitation 2. By the admixture of two or more liquid ingredients
Classes of Elixirs
1. Non-medicated - used in the extemporaneous filling of prescriptions involving 1. The addition of a therapeutic agent to a pleasant tasting vehicle 2. The dilution of an existing medicated elixir NOTE: There should be no incompatibilities between the above and the component of the formula Example: Aromatic elixirs, Compound Benzaldehyde Elixir, Iso alcoholic Elixir
2. Medicated Elixirs are employed for the therapeutic benefit of the medicinal agent present. Example: 1. Phenobarbital elixir= Phenobarbital 4g; Orange oil 0.25mL; Propylene Glycol 100mL; Alcohol 200mL; Sorbitol Solution 600m; Color q.s purified water to make 1000mL.
The official and commercial elixirs contain a single therapeutic agent except : Terpene hydrate and Codein Elixir The advantage of Single therapeutic agent: Dosage taken may be increased or decreased by taking more or less of the elixir without much problem. Examples: Antihistamine Elixir; Hypnotic and Sedative Elixirs (Barbital) 2. Theophylline Elixir: Theophylline 5.3g; Citric Acid 10g; Liquid Glucose 44g; Syrup 132.0mL; Glycerin 50mL; Sorbitol Solution 324mL; yellow No. 5 0.1g; purified water to make 100mL 3. Diphenhydramine Hydrochloride Elixir: Diphenhydramine HCl 2.5g; Orange oil 0.24mL; Cinnamon oil 0.11mL; Clove oil 0.08mL; Coriander oil 0.03mL; Anethole 0.03mlL; Amaranth solution 1.6 mL; alcohol 350 mL; Purified water, q.s to make 1000 mL
Example Formulations for some non-medicated elixirs 1. Aromatic elixir: Compound Orange spirit 12mL; Syrup 375mL; Talc 30g; Alcohol and purified water to make 1000mL 2. Compound Benzaldehayde Elixir: Benzaldehyde 0.5mL; Syrup 400mL; Purified water, q.s to make 1000mL 3. Iso-alcoholic elixir contains low and high alcoholic 1. Low alcoholic- Compound orange spirit 10mL; Alcohol 100mL; Glycerin 200mL; Sucrose 320mL; Purified water q.s to make 1000mL 2. High Alcoholic- Compound orange spirit 4mL; Saccharin 3g; Glycerin 200mL; Alcohol, q.s to make 1000mL
2. 3. 4. 5. 6. 7.
Analgesic/Antipyretic
Acetaminophen Elixir- Childrens Tylenol Elixir
Anticholinergic/Antispasmodic
Hyscyamine Sulfate Elixir Levsin Elixir
Antiasthma
Diphenhydramine HCl Benadryl Elixir
Antipsychotic
Fluphenazine HCl Fluphenazine HCl
Cardiotonic
Digoxin Lanoxin Pediatric Elixir
Sedative/Hypnotics
Butabarbital Sodium- Butisol Sodium Phenobarbital Phenobarbital Elixir
GLYCERITES
Solutions of mixtures of medicinal or pharmaceutical substances in glycerin
Characteristics: 1. Generally a minimum of 50% of glycerin is present in glycerites 2. Due to high concentration of glycerin and the presence of large amount of dissolved or undissolved substances. Glycerites are generally quite viscous with some of them reaching a jelly like consistency 3. Glycerites are considered to be stable preparation and are not usually as prone to microbial contamination because it possesses preservative properties
Examples of Glycerites
1. Starch Glycerite Glyceratum Amyli; starch glycerin- used as an emollient; starch 100g; water 200mL;Benzoic acid 2g; Glycerin 700mL 2. Tannic acid Glycerite - as an astringent Tannic acid 20g; Exsiccated Sodium sulfite 02.g and Sodium citrate 1g; Glycerin q.s to make 1000g 3. Phenol Glycerite - 40mL is official in BPC diluted with Glycerin q.s 100mL
4. Boroglycerin Glycerite antibacterial 5. Iodine and Zinc Iodide Glycerite Glyceritum Iodi et Zinci Iodi 6. Tragacanth Glycerite Glyceratum Tragacanthae Storage of Glycerites Glycerites are hygroscopic, therefore, should be stored in tightly closed containers.
MIXTURES
Are aqueous liquid preparations which contains suspended insoluble solid substances and are intended for external use
Characteristics: 1. Should have finely divided particles to suspend more readily and settle out much slowly than larger particles thus uniform dosage. 2. The more nearly colloidal it is better as protective and adsorbent on inflamed surfaces. 3. Palatability associated with colloidal agents ***mixtures should have shake well label
Paregoric
Alcohol Glycerin Purified water q.s. to make
120 mL
30 mL 120 mL 1000 mL.
200g
10 g 5g 2g 1g 20 mL 0.75 mL 1000 mL
EXTRACTIVES
Extraction involves the separation of medicinally active portions of plant or animal tissues from the inactive components through the use of selective solvents Galenicals include classes of preparations knows as: 1. Decoction 2. Infusion 3. Fluidextracts 4. Tinctures 5. Pilular (semi solid) extracts 6. Powdered extracts
Methods of Extraction
1. Maceration term derived from latin word macerare meaning to soak. Process in which the properly comminuted drug is permitted to soak in the menstruum and the soluble constituents are dissolved Examples: (Process M) Compound Benzoin, Sweet orange Peel Tincture; Compound Cardamon; Tolu Balsam Tincture
The choice of type of Percolator depends upon 1. Nature of the drug 2. Type of product prepared 3. Quantity of drug to be extracted Processes and steps of Percolation 1. Preparation of the dried crude drug for percolation a. Powdering b. Moistening 2. Packing the percolator 3. Period of Maceration 4. Percolation and collection of percolate 5. Adjustment of concentration of percolation as required
Methods of Extraction
3. Digestion form of maceration with gentle heat 4. Infusion process in which vegetable drugs, generally coarsely comminuted, are extracted of the water-soluble constituents 5. Decoction process of boiling vegetable substances with water to extract the soluble principles
EXTRACTS
Are concentrated preparations of vegetable or animal drugs obtained by removal of the active constituents of the respective drugs with suitable menstruum, evaporation of all or nearly all the solvents, and adjustment of the residual masses or powders to the prescribed standards.
Methods of Preparation Prepared by percolation then evaporation off the solvent either by distillation under pressured and using reduced heat.
TINCTURES Are defined as alcoholic or hydro alcoholic solution prepared from vegetable material or from chemical substance.
Examples Of Solutions Applied Topically 1. Aluminum acetate - Aqueous vehicle Astringent (Burows Solution) 2. Aluminum Subacetate - Aqueous vehicle Astringent (Modified Burows) 3. Calcium Hydroxide - Aqueous vehicle Astringent - (Lime Water; Liquor Calcis) 4. Coal Tar - Alcoholic vehicle - Antieczematic, antipsoriatic (Liquor Carbonis Detergens: Liquor Picis carbonis; LCD) 5. Hydrogen Peroxide Topical Solution - Aqueous vehicle - Anti-infective (Peroxide)
6. Chlorhexidine Gluconate Solution - for skin wound and general skin cleanser, surgical scrub, and preoperative skin preparation, effective in gram negative and positive such as Pseudomonas aeruginosa 7. Povidone-Iodine - Aqueous vehicle - Anti-infective (Betadine Solution) 8. Thimerosal - Aqueous vehicle - Antibacterial and fungistatic (Merthiolate Solution) Examples Of Tinctures Applied Topically mild
1. Green soap Tincture - Alcohol vehicle - Detergent. Also contains 2% lavender oil as perfume 2. Iodine Tincture - Alcohol - water vehicle - Anti-infective 3. Compound Benzoin Tincture - alcohol - Topical protectant
Preparation of Tinctures
1. Maceration Examples: Compound Benzoin Tinctures; Sweet Orange Peel Tincture and ToLu Balsam Tincture 2. Percolation Examples: Belladona Tincture and Vanilla Tincture
Alcohol Content
Tinctures are considered to be stable preparation containing alcohol to protect against microbial growth. Green soap Tincture - 28 to 32% alcohol Tolu Balsam Tincture - 77 to 83% alcohol Pharmaceutical Uses As flavoring tinctures like vanilla, sweet orange peel, Tolu balsam tinctures. Medicinal use - Iodine Tincture, Thimerosal, Nitromersol Tinctures - Anti-infective; Compound Benzoin Tincture - Topical protectant; Green soap Tincture - Topical detergent; Paregoric Tincture - Antiperistalsis; Belladona Tincture - Anticholinergic
Disadvantages of Tinctures
1. Unpleasant tasting 2. Physician will prefer single drug instead of preparation from plants 3. High alcohol content
FLUIDEXTRACT Are liquid preparations of vegetable drugs containing alcohol as a solvent or as a preservative or both, and so made that each mL contains the therapeutic constituents of 1g of the standard drug that it represents
Characteristics of Fluidextract
1. Because they contain alcohol and are highly concentrated, fluidextracts are sometimes referred to as 100% tinctures 2. Fluidextracts of potent drugs are ten times as concentrated or as potent as corresponding tincture Example: Belladonna Tincture is 0.6mL while its fluidextract is 0.06mL
Disadvantages of Fluidextract 1. Because of their concentrated nature, many fluidextracts are considered too potent for safe self administration 2. Too bitter tasting or otherwise unpalatable
Preparations of Fluidextracts Percolation is preferred in all cases because of the exhaustive extraction required.
3 Processes labeled A, D, or B and C or E Process A - entails exhaustive percolation with an alcoholic or
hydroalcoholic menstruum. Example: Senna Fluidextract
with boiling water as the menstruum and alcohol generally added to the concentrated percolate as preservative. A heat resistant or metallic percolator is used.
Official Preparation
1. Glycyrrhiza Fluidextract - Licorice root Fluidextract - flavoring agent 2. Eriodictyon Fluidextract - Yerba Santa Fluidextract - cathartic 3. Cascara Sagrada Fluidextract Rhamnus Purshiana Fluidextract 4. Aromatic Cascara Sagrada Fluidextract
NASAL PREPARATIONS Are aqueous preparations rendered isotonic to nasal fluids and stabilized and preserved as required
Example of Some Nasal Preparations 1. Afrin Nasal Spray/drops- Oxymetazone- Nasal decongestant 2. Beconase AQ Nasal Spray- Beclomethasone diproprionatesynthetic corticosteroid 3. Diapid Nasal Spray Lopressin- Antidiuretic, prevention of diabetes 4. Nasalcrom spray Cromolyn- allergic rhinitis
5. Ocean Mist isotonic sodium chloride- restore moisture/relieve dry inflamed nasal 6. Privine HCl solution- Naphazoline HCl- nasal adrenergic 7. Syntocinon Spray Oxytocin -synthetic, preparatory to breast feeding
8. Neo-Syneprine Oxymethazoline HCl- nasal adrenergic 9. Nasalide Nasal Solution- Flunisolide parennial/seasonal rhinitis OTIC SOLUTIONS
As sometimes referred to as ear or Aural preparations preparations frequently used in the ear, with suspensions or ointments also finding some application. Usually placed in the ear canal by drops or small amounts for the removal of excessive cerumen (ear wax), or treatment of ear infections, inflammation or pain.
Examples of Some Commercial Otic Solutions 1. Americaine- Benzocaine Local anesthetic
2. Auralgan- Antipyrine, Benzocaine Acute Otitis Media 3. Cerumenex drops Triethanolamine Cerumenolytic agent;
removes impacted earwax
4. Chloromycetin Chloramphenicol Anti-infective 5. Cortisporin Solution Polymyxin B sulfate- antibacterial 6. Debrox Drops- Carbamide Peroxide Ear wax removal 7. PediOtic - Polymyxin B sulfate, neomycin sulfate Antibacterial
8. Metreton - Prednisolone sodium phosphate Antiinflammatory
DOUCHES
A douche is an aqueous solutions which is directed against a part or into a cavity of the body. It functions as a cleansing or antiseptic. Characteristics Douches are usually directed to the appropriate body parts by using Bulb syringe. Example: vaginal syringe is made up of an 8 to 10 ounce capacity bulb syringe with a large vulcanite or rubber spray tube.
KINDS OF DOUCHES
1. Eye Douche - used to removed foreign particles and discharges from the eyes, is directed gently at an oblique angle and is allowed to run from the inner to outer corner of the eye. 2. Pharyngeal Douche - are used to prepare the interior of the throat for an operation and to cleanse it in suppurative conditions (formation of discharge of pus). 3. Nasal Douche - used to cleanse nasal passage 4. Vaginal Douche - used for irrigative cleansing of the vagina therefore for hygienic effects, also called urethral douche or irrigation
Characteristics
Douches are more frequently dispensed in the form of powder with directions for dissolving in a specified quantity of water, usually warm Dobells Solution Tablets (Compound Sodium Borate Solution NF) used for nasal or pharyngeal douches.
Douches are not official as a class of preparations but general substances in the USP and NF are frequently employed as such in weak solution. Example: Benzalkonium Chloride used in various douches
ENEMAS
Enemas are also known as CLYSTER, they are rectal injections employed to:
Characteristics:
Enemas are usually given at body temperature in quantities of 1 to 2 pints injected slowly with enema syringe. If they are to be retained in the intestine, they should not be used in larger quantities than 6 fluid ounces for an adult.
Examples:
1. Enema of soft soap - prepared by dissolving 50 g of soft soap with purified water to make 1000 mL.
Example
Preparation: Barium Sulfate Enema Synonym: Barium Salt Latin Name : Baric Sulfae Formula : Barium Sulfate Acacia Mucilage Starch Enema, q.s 120 g 100 mL
To make
500 mL
Procedure: Prepared by mixing Barium Sulfate (120 g) with 100 mLof acacia mucilage and sufficient Starch Enema to make 500 mL Starch Enema is made by triturating 30 g of powdered starch with 200 mL cold water then sufficient quantity of water added to make 1 Liter. Use: For diagnostic visualization of GIT
2 Types Of Enema
1. Evacuation Enemas - are rectal enemas employed to
promote evacuation of bowel and to cleanse the colon for retention and for diagnosis. Available in disposable plastic squeeze bottles containing a pre measured amount of enema solution. The agents present are solutions of sodium phosphate, sodium biphosphate, glycerin and docusate potassium and light mineral oil.
Types Of Retention Enema 1. Nutritive Enema - supply nutrient to the patient 2. Medicated Enema - supply medication for systemic effect 3. Disgnostic Enema - BaSO4 and Fleet Enema Other Enemas 1. Aminophylline Enema - NLT 90% and NMT 110% of C6H24N10 . 2H2O 2. Methyl Prednisolone Acetate - NLT 90% and NMT 110% of C24H32O6 3. Cortisol Enema - NLT 90% and NMT 110% of C21H30O5
2.
Isopropyl Rubbing Alcohol is about 70% by volume of isopropyl alcohol, the remainder consisting of water with or without color additives, stabilizers, and perfume oils.
Uses: as rubefacient and soothing rub; 91% isopropyl alcohol - employed by diabetic patients in preparing needles and syringes for hypodermic injections of insulin and for disinfecting the skin
3. Hexachlorophene Liquid Cleanser - is an antibacterial sudsing emulsion containing colloidal dispersion of hexachlorophene 3% W/W in a stable emulsion consisting of entsufon sodium (synthetic detergent), petrolatum,lanolin cholesterols, methylcellulose, polyethylene glycol, PG monostearate, lauryl myristyl diethanolamide, sodium benzoate and water Uses: bacteriostatic cleansing agent, surgical scrub
LINIMENTS
Are alcoholic or oleaginous solutions or emulsions of various medicinal substances intended for external application to the skin, generally with rubbing. Formerly called embrocations for substance applied with rubbing.
Alcoholic liniment - used as rubefacient ( induce mild irritation with reddening of the skin), counterirritant, mildly astringent, and penetrating effect.
Oily liniment are milder in action and less irritating to the skin than the alcoholic, used as protective coating and use as rubefacient for muscular pain
Components of Liniments
1. Counterirritant 2. Antiseptic 3. Local Anesthetics 4. Analgesics
Methods of Preparation
Liniments are prepared in the same manner as solutions, emulsions or suspensions
oil
2. Solubility of the desired components in the various solvents. For oleaginous liniments the solvents may be fixed oil, almond oil, peanut oil, sesame oil or cotton seed oil or volatile oil such as wintergreen or turpentine oil or combination of fixed or volatile oil. NOTE: There are presently no official liniments in the USP and NF
Oleic acid
Turpentine oil Water
85.0 mL
250.0 mL 625.0 mL
Mix oleic acid with the turpentine oil, add the diluted Ammonia mixed with 45 mL of previously warmed water. Shake. Dissolve the ammonium chloride in the remainder of the water, add to the emulsion and mix.
Oleic acid
Arachic oil
5 mL
500 mL
Ca(OH)2 solution to make 1000 mL Triturate the calamine with the wool fat, the arachis oil and oleic acid, previously melted together. Transfer to a suitable container, add the Ca(OH)2 solution and shake vigorously.
CAMPHOR LINIMENT
Linimentum Camphoras; Camphorated Oil Camphor Cottonseed oil to make 200 g 800 g 1000 g
Place the cottonseed oil into a suitable dry flash or bottle, heat on the steam bath. Add camphor and stopper the container securely. Agitate to dissolve the camphor without further heating.